Table 3.

Ongoing clinical trials using targeted therapiesa

TreatmentTargetsClinical trial phaseNumber of trials
Biomarker driven
 BGJ398FGFR, ABL, FYN, KIT, LCK, LYN, YESII1
 Ponatinib hydroclorideBCR-ABL, VEGFR, PDGFR, FGFR, EPH, SRC, KIT, RET, TIE2, FLT3II1
 AG-221Mutated IDH2I/II1
 AG-120Mutated IDH1I1
Monotherapy
 Cabozantinib (XL-184)MET, VEGFR2, RET, c-KIT, FLT1/3/4, TIE2II1
 EverolimusmTORII2
 SunitinibVEGFR, PDGFR, KIT, FLT3, RETII1
 RegorafenibRET, RAF-1, VEGFR, KIT, BRAF (V600E), PDGFRB, FGFR1, TIE2II2
 CelecoxibCOXIV1c
 TrastuzumabHER2-neuII1
 LY2801653c-MET, MST1R, FLT3, AXL, MERTK, TEK, ROS1, DDR1/2I1
 BKM120VPS34/mTOR/DNAPK/PI4KβII1
 LapatinibErbB2-4/EGFR/SRCII2
 SelumetinibMEK1/2II1
 MK2206AKT1-3II1
 RAV12RAAG12I1
 PLX8394BRAFI/II1
Combination
 Selumetinib + MK-2206MEK1 + AKT1-3II1
 Bosutinib + capecitabineABL/SRC/c-KITI1
 AZD2171 + AZD0530VEGFR/PDGFR/FGFR1/c-KIT + SRC/ABL/LCK/YES/EGFR/LYNI1
 Pazopanib + GSK1120212VEGFR/PDGFR/FGFR/KIT + MEK1/2I1
 Cetuximab + erlotinibEGFRI/II2c
 Trastuzumab + tipifarnibHER2-neu + FTII1
 Erlotinib + bevacizumabEGFR + VEGFAII2
Combination with chemotherapy
 Radiotherapy + bevacizumabVEGFAI1
 Chemotherapyb + veliparibPARP1/2I1
 Chemotherapy + bevacizumabVEGFAII2c
 Chemotherapy ± panitumumabEGFRII5c
 Chemotherapy ± vandetanib (ZD6474)VEGFR, EGFRI, II2c
 Chemotherapy + cediranibVEGFRII1
 Chemotherpy ± sorafenibBRAF, VEGFR, PDGFRI/II2
 Chemotherapyb ± cetuximabEGFRII2c
 Chemotherpyb + selumetinibMEK1/2I/II1
 Chemotherpy ± trametinibMEK1/2II1
 Chemotherapyb + sirolimusmTORI1
 Chemotherapy + pazopanibVEGFR/PDGFR/FGFR/KITII1
 Chemotherapy + AZD2171VEGFR/PDGFR/FGFR1/c-KITII1
 Chemotherapyb ± CX-4945CX2I/II1c
 Chemotherapy + erlotinibEGFRI/II3

Abbreviations: FGFR, fibroblast growth factor; KIT, c-kit proto-oncogene receptor tyrosine kinase; PDGFR, platelet-derived growth factor receptor.

  • aInformation acquired from clinicaltrials.gov.

  • bChemotherapy (standard of practice: gemcitabine and cisplatin).

  • cRandomized controlled clinical trials.